2. Cell Cycle/DNA Damage Stem Cell/Wnt MAPK/ERK Pathway JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Casein Kinase ERK Pim DYRK Apoptosis
  4. CK2/ERK8-IN-1

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.

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CK2/ERK8-IN-1 Chemical Structure

CK2/ERK8-IN-1 Chemical Structure

CAS No. : 1085822-09-8

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Customer Review

Based on 1 publication(s) in Google Scholar

CK2/ERK8-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

View All Isoforms
CK1 CK2

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All Pim Isoform Specific Products:

View All Isoforms
PIM1 PIM2 PIM3

View All DYRK Isoform Specific Products:

View All Isoforms
DYRK1 DYRK2 DYRK3 DYRK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].

IC50 & Target

CK2

0.5 μM (IC50)

CK2

0.25 μM (Ki)

ERK8

0.5 μM (IC50)

PIM1

8.65 μM (Ki)

HIPK2

15.25 μM (Ki)

DYRK1A

11.9 μM (Ki)

Apoptosis

 

In Vitro

CK2/ERK8-IN-1 (Compound K66; 0-50 µM; 24 hours; Jurkat cells) treatment displays cytotoxic activity in Jurkat cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CK2/ERK8-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: Jurkat cells
Concentration: 0-50 µM
Incubation Time: 24 hours
Result: Inhibited cell growth in a dose-dependent manner.
Molecular Weight

534.82

Formula

C11H9Br4N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CN1C2=C(Br)C(Br)=C(Br)C(Br)=C2N=C1N(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (31.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8698 mL 9.3489 mL 18.6979 mL
5 mM 0.3740 mL 1.8698 mL 3.7396 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1.67 mg/mL (3.12 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.67 mg/mL (3.12 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥99.0%

COA (256 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8698 mL 9.3489 mL 18.6979 mL 46.7447 mL
5 mM 0.3740 mL 1.8698 mL 3.7396 mL 9.3489 mL
10 mM 0.1870 mL 0.9349 mL 1.8698 mL 4.6745 mL
15 mM 0.1247 mL 0.6233 mL 1.2465 mL 3.1163 mL
20 mM 0.0935 mL 0.4674 mL 0.9349 mL 2.3372 mL
25 mM 0.0748 mL 0.3740 mL 0.7479 mL 1.8698 mL
30 mM 0.0623 mL 0.3116 mL 0.6233 mL 1.5582 mL
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CK2/ERK8-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CK2/ERK8-IN-11085822-09-8Casein KinaseERKPimDYRKApoptosisExtracellular signal regulated kinasesPim kinasesDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseCK2ERK8PIM1HIPK2DYRK1Acytotoxicbenzimidazolepro-apoptoticMAPK15ERK7Inhibitorinhibitorinhibit

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